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用于提高姜黄素口服生物利用度的聚合物纳米颗粒

Polymeric Nanoparticles for Increasing Oral Bioavailability of Curcumin.

作者信息

Umerska Anita, Gaucher Caroline, Oyarzun-Ampuero Felipe, Fries-Raeth Isabelle, Colin Florence, Villamizar-Sarmiento María Gabriela, Maincent Philippe, Sapin-Minet Anne

机构信息

Université de Lorraine, CITHEFOR, F-54000 Nancy, France.

Departamento de Ciencias y Tecnología Farmacéuticas, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, 758-0150 Santiago, Chile.

出版信息

Antioxidants (Basel). 2018 Mar 24;7(4):46. doi: 10.3390/antiox7040046.

Abstract

Despite the promising biological and antioxidant properties of curcumin, its medical applications are limited due to poor solubility in water and low bioavailability. Polymeric nanoparticles (NPs) adapted to oral delivery may overcome these drawbacks. Properties such as particle size, zeta potential, morphology and encapsulation efficiency were assessed. Then, the possibility of storing these NPs in a solid-state form obtained by freeze-drying, in vitro curcumin dissolution and cytocompatibility towards intestinal cells were evaluated. Curcumin-loaded Eudragit RLPO (ERL) NPs showed smaller particle diameters (245 ± 2 nm) and better redispersibility after freeze-drying than either poly(lactic--glycolic acid) (PLGA) or polycaprolactone (PCL) NPs. The former NPs showed lower curcumin encapsulation efficiency (62%) than either PLGA or PCL NPs (90% and 99%, respectively). Nevertheless, ERL NPs showed rapid curcumin release with 91 ± 5% released over 1 h. The three curcumin-loaded NPs proposed in this work were also compatible with intestinal cells. Overall, ERL NPs are the most promising vehicles for increasing the oral bioavailability of curcumin.

摘要

尽管姜黄素具有良好的生物学和抗氧化特性,但其在医学上的应用因在水中溶解度低和生物利用度低而受到限制。适用于口服给药的聚合物纳米颗粒(NPs)可能会克服这些缺点。评估了粒径、zeta电位、形态和包封率等性质。然后,评估了通过冷冻干燥获得的这些NPs以固态形式储存的可能性、体外姜黄素溶解情况以及对肠道细胞的细胞相容性。负载姜黄素的Eudragit RLPO(ERL)NPs在冷冻干燥后的粒径较小(245±2 nm)且再分散性优于聚(乳酸-乙醇酸)(PLGA)或聚己内酯(PCL)NPs。前者的NPs姜黄素包封率(62%)低于PLGA或PCL NPs(分别为90%和99%)。然而,ERL NPs姜黄素释放迅速,1小时内释放91±5%。这项工作中提出的三种负载姜黄素的NPs也与肠道细胞相容。总体而言,ERL NPs是提高姜黄素口服生物利用度最有前景的载体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7e2b/5946112/66893298c60b/antioxidants-07-00046-g001.jpg

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